KU-0060648 [Ligand Id: 8011] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1086377
  • protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase catalytic subunit in Human [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform in Human [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform in Human [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform in Human [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform in Human [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736]
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  • ATM serine/threonine kinase/Serine-protein kinase ATM in Human [ChEMBL: CHEMBL3797] [GtoPdb: 1934] [UniProtKB: Q13315]
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  • ATR checkpoint kinase/Serine/threonine-protein kinase ATR in Human [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535]
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  • mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345]
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  • Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
protein kinase, DNA-activated, catalytic subunit/DNA-dependent protein kinase catalytic subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3142] [GtoPdb: 2800] [UniProtKB: P78527]
GtoPdb - - 8.3 pIC50 5 nM IC50 J Med Chem (2013) 56: 6386-401 [PMID:23855836]
ChEMBL Inhibition of DNA-dependent protein kinase B 8.3 pIC50 5 nM IC50 Bioorg Med Chem Lett (2010) 20: 3649-3653 [PMID:20472428]
ChEMBL Inhibition of DNA-PK B 8.3 pIC50 5 nM IC50 Bioorg Med Chem Lett (2011) 21: 966-970 [PMID:21216595]
ChEMBL Inhibition of DNA-PK B 8.3 pIC50 5 nM IC50 Bioorg Med Chem Lett (2012) 22: 5352-5359 [PMID:22835870]
ChEMBL Inhibition of DNA-PK B 8.3 pIC50 5 nM IC50 Eur J Med Chem (2012) 57: 85-101 [PMID:23059543]
ChEMBL Inhibition of human DNA-PK using GST-tagged p53N66 as substrate after 1 hr by ELISA-based chemiluminiscence assay B 8.3 pIC50 5 nM IC50 J Med Chem (2013) 56: 6386-6401 [PMID:23855836]
ChEMBL Inhibition of DNA-PK autophosphorylation at S2056 in human HeLa cells B 6.87 pEC50 136 nM EC50 J Med Chem (2013) 56: 6386-6401 [PMID:23855836]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336]
ChEMBL Inhibition of PI-3K alpha (unknown origin) B 8.4 pIC50 4 nM IC50 J Med Chem (2013) 56: 6386-6401 [PMID:23855836]
GtoPdb - - 8.4 pIC50 4 nM IC50 J Med Chem (2013) 56: 6386-401 [PMID:23855836]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338]
GtoPdb - - 9.3 pIC50 0.5 nM IC50 J Med Chem (2013) 56: 6386-401 [PMID:23855836]
ChEMBL Inhibition of PI-3K beta (unknown origin) B 9.3 pIC50 0.5 nM IC50 J Med Chem (2013) 56: 6386-6401 [PMID:23855836]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329]
GtoPdb - - 10 pIC50 <0.1 nM IC50 J Med Chem (2013) 56: 6386-401 [PMID:23855836]
ChEMBL Inhibition of PI-3K delta (unknown origin) B 10 pIC50 <0.1 nM IC50 J Med Chem (2013) 56: 6386-6401 [PMID:23855836]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736]
ChEMBL Inhibition of PI-3K gamma (unknown origin) B 6.23 pIC50 590 nM IC50 J Med Chem (2013) 56: 6386-6401 [PMID:23855836]
GtoPdb - - 6.23 pIC50 590 nM IC50 J Med Chem (2013) 56: 6386-401 [PMID:23855836]
ATM serine/threonine kinase/Serine-protein kinase ATM in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3797] [GtoPdb: 1934] [UniProtKB: Q13315]
ChEMBL Inhibition of ATM (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2013) 56: 6386-6401 [PMID:23855836]
ATR checkpoint kinase/Serine/threonine-protein kinase ATR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5024] [GtoPdb: 1935] [UniProtKB: Q13535]
ChEMBL Inhibition of ATR (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2013) 56: 6386-6401 [PMID:23855836]
mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345]
ChEMBL Inhibition of mTOR (unknown origin) B 5 pIC50 10000 nM IC50 J Med Chem (2013) 56: 6386-6401 [PMID:23855836]
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG expressed in cisapride treated CHO cells by Ion Works assay B 4.7 pIC50 >20000 nM IC50 J Med Chem (2013) 56: 6386-6401 [PMID:23855836]

ChEMBL data shown on this page come from version 36:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]